Zobrazeno 1 - 4
of 4
pro vyhledávání: '"Andrew Stephen Robert Jennings"'
Autor:
Wayne F. A. Sheppard, David S. Reynolds, Alison J. Smith, John R. Atack, Joanna Stanley, David James Hallett, Richard Thomas Lewis, Keith A. Wafford, Rowan A. Wilson, Timothy Blackburn, George R. Marshall, Wesley Peter Blackaby, Andrew Pike, Spencer J. Tye, Andrew Stephen Robert Jennings, Susan M. Cook, Pushpinder Ferris, Bindi Sohal
Publikováno v:
Journal of Medicinal Chemistry. 49:2600-2610
The development of a series of GABA(A) alpha2/alpha3 subtype selective pyridazine based benzodiazepine site agonists as anxiolytic agents with reduced sedative/ataxic potential is described, including the discovery of 16, a remarkably alpha3-selectiv
Autor:
George R. Marshall, Rachael Lincoln, Richard Thomas Lewis, Bindi Sohal, Susan M. Cook, Keith A. Wafford, John R. Atack, David James Hallett, Alison J. Smith, David S. Reynolds, Spencer J. Tye, Leslie J. Street, Michael G. N. Russell, Andrew Stephen Robert Jennings, Andrew Pike, José L. Castro, Joanna Stanley, Wayne F. A. Sheppard
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:1477-1480
Imidazo[1,2-a]pyrimidines and imidazo[1,2-b][1,2,4]triazines are ligands for the benzodiazepine binding site of GABA(A) receptors that are functionally selective for the alpha2/alpha3 subtypes over the alpha1 subtype. SAR studies to optimise this fun
Autor:
H. Donald Burns, Martin R. Guscott, Andrew Stephen Robert Jennings, Sarah Almond, Simon Charles Goodacre, Gopalan V. Pillai, Alison J. Smith, Richard Thomas Lewis, Christine Ryan, Angus Murray Macleod, Andrew Pike, Leslie J. Street, Jacquelynn J. Cook, Steve Thomas, Terence G. Hamill, Suzanne Wood, Terry A. Brown, Wesley Peter Blackaby, Wai-Si Eng, Joanne Thomson
Amalgamation of the structure−activity relationship of two series of GlyT1 inhibitors developed at Merck led to the discovery of a clinical candidate, compound 16 (DCCCyB), which demonstrated excellent in vivo occupancy of GlyT1 transporters in rhe
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cfc2feaa39772a8555e55e31bcedea20
https://europepmc.org/articles/PMC4007840/
https://europepmc.org/articles/PMC4007840/
Autor:
Richard Thomas Lewis, Leslie J. Street, Alison J. Smith, Terry A. Brown, Joanne Thomson, Gopalan V. Pillai, Simon Charles Goodacre, Steve Thomas, Andrew Stephen Robert Jennings, Wesley Peter Blackaby, Andrew Pike
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(8)
Spleen tyrosine kinase (SYK) is a non-receptor cytosolic kinase. Due to its pivotal role in B cell receptor and Fc-receptor signaling, inhibition of SYK has been targeted in a variety of disease areas. Herein, we report the optimization of a series o